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Assay Detail

CHEMBL4031179

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Binding
Binding affinity to human cGAS (2 to 522 residues) expressed in Sf9 insect cells by surface plasmon resonance assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cyclic GMP-AMP synthase (CHEMBL4105728)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of PF-06928215 as a high affinity inhibitor of cGAS enabled by a novel fluorescence polarization assay.
Hall J, Brault A, Vincent F, Weng S, Wang H, Dumlao D, Aulabaugh A, Aivazian D, Castro D, Chen M, Culp J, Dower K, Gardner J, Hawrylik S, Golenbock D, Hepworth D, Horn M, Jones L, Jones P, Latz E, Li J, Lin LL, Lin W, Lin D, Lovering F, Niljanskul N, Nistler R, Pierce B, Plotnikova O, Schmitt D, Shanker S, Smith J, Snyder W, Subashi T, Trujillo J, Tyminski E, Wang G, Wong J, Lefker B, Dakin L, Leach K.
PLoS One (2017) 12 : e0184843 -null
PubMed 28934246 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 6 5.29 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4096573 1 6.70
CHEMBL4084664 1 5.57
CHEMBL4062994 1 5.17
CHEMBL4103560 1 4.90
CHEMBL4085628 1 4.11
CHEMBL4065757 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4096573 Kd = 200.0 nM 6.70
CHEMBL4084664 Kd = 2700.0 nM 5.57
CHEMBL4062994 Kd = 6700.0 nM 5.17
CHEMBL4103560 Kd = 12500.0 nM 4.90
CHEMBL4085628 Kd = 78000.0 nM 4.11
CHEMBL4065757 Kd = 171000.0 nM -